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Assay Detail

CHEMBL1015345

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Binding
Selectivity assessed as difference in pEC50 for human cloned beta2 adrenergic receptor and pEC50 for human cloned beta3 adrenergic receptor
18
Total Activities
18
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.
Procopiou PA, Barrett VJ, Bevan NJ, Biggadike K, Butchers PR, Coe DM, Conroy R, Edney DD, Field RN, Ford AJ, Guntrip SB, Looker BE, McLay IM, Monteith MJ, Morrison VS, Mutch PJ, Richards SA, Sasse R, Smith CE.
J Med Chem (2009) 52 : 2280 -2288
PubMed 19317397 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 17 4.00 4.00
pEC50 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL446840 1 4.00
CHEMBL475237 1 -
CHEMBL475389 1 -
CHEMBL516056 1 -
CHEMBL474393 1 -
CHEMBL514032 1 -
CHEMBL500782 1 -
CHEMBL506518 1 -
CHEMBL456485 1 -
CHEMBL475236 1 -
CHEMBL485847 1 -
CHEMBL483202 1 -
CHEMBL483407 1 -
CHEMBL443435 1 -
CHEMBL1263 SALMETEROL 4.0 1 -
CHEMBL1256786 FORMOTEROL 4.0 1 -
CHEMBL520313 1 -
CHEMBL434 ISOPROTERENOL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL446840 EC50 = 100000.0 nM 4.00
CHEMBL475237 EC50 = 630957.34 nM -
CHEMBL475389 EC50 = 398107.17 nM -
CHEMBL516056 EC50 = 794328.23 nM -
CHEMBL474393 EC50 = 1584893.19 nM -
CHEMBL514032 EC50 = 1584893.19 nM -
CHEMBL500782 EC50 = 3981071.71 nM -
CHEMBL506518 EC50 = 6309573.44 nM -
CHEMBL456485 EC50 = 1995262.31 nM -
CHEMBL475236 EC50 = 501187.23 nM -
CHEMBL485847 EC50 = 7943282.35 nM -
CHEMBL483202 EC50 = 3162277.66 nM -
CHEMBL483407 pEC50 - -
CHEMBL443435 EC50 = 794328.23 nM -
CHEMBL1263 SALMETEROL EC50 = 199526.23 nM -
CHEMBL1256786 FORMOTEROL EC50 = 19952623.15 nM -
CHEMBL520313 EC50 = 1584893.19 nM -
CHEMBL434 ISOPROTERENOL EC50 = 1000000000.0 nM -